ChemicalBook CAS DataBase List 1000023-05-1

1000023-05-1

Name	4H-1-Benzopyran-4-one, 2-[2-chloro-4-(trifluoromethyl)phenyl]-5,7-dihydroxy-8-[(2R,3S)-2-(hydroxymethyl)-1-methyl-3-pyrrolidinyl]-, hydrochloride (1:1)
CAS	1000023-05-1
Molecular Formula	C22H20Cl2F3NO5
Molecular Weight	506.3
MOL File	1000023-05-1.mol

Chemical Properties

storage temp.	4°C, away from moisture
solubility	DMSO : ≥ 250 mg/mL (493.78 mM)
form	Solid
color	Light yellow to yellow

Hazard Information

Uses

Voruciclib hydrochloride is an orally active and selective CDK inhibitor with Ki values of 0.626 nM-9.1 nM. Voruciclib hydrochloride potently blocks CDK9, the transcriptional regulator of MCL-1. Voruciclib hydrochloride represses expression of MCL-1 in multiple models of diffuse large B-cell lymphoma (DLBCL)[1].

in vivo

Combination of Voruciclib hydrochloride (200 mpk; Oral gavage) and Venetoclax (10 mpk, 1 mpk, 50 mpk, 25 mpk in U2932, RIVA, SU-DHL-4 and NU-DHL-1, respectively) leads to enhance tumor growth inhibition compared to either drug alone in U2932, RIVA, SU-DHL-4 (six days per week for 4 weeks), and NU-DHL-1 models (five days per week for 3 weeks) of DLBCL^[1].

Animal Model:	ABC subtypes (U2932, RIVA, OCI-LY10), GCB subtypes (SU-DHL-4, NU-DHL-1) xenografted in Female NOD.CB17-Prkdcscid/NCrHsd mice^[1]
Dosage:	200 mpk
Administration:	Oral gavage; U2932, RIVA, SU-DHL-4 (six days per week for 4 weeks), OCI-LY10 (six days per week for 2 weeks), NU-DHL-1 (five days per week for 3 weeks)
Result:	Enhanced tumor growth inhibition in U2932, RIVA, SU-DHL-4 and NU-DHL-1 models except in OCI-LY10 model.

IC 50

CDK9/CycT1: 1.68 nM (Ki); CDK9/cyc T2: 0.626 nM (Ki); CDK6/cycD1: 2.92 nM (Ki); CDK4/Cyc D1: 3.96 nM (Ki); CDK1/cycB: 5.4 nM (Ki); CDK1/cyc A: 9.1 nM (Ki)

storage

4°C, away from moisture

References

[1] Dey J, et al. Voruciclib, a clinical stage oral CDK9 inhibitor, represses MCL-1 and sensitizes high-risk Diffuse Large B-cell Lymphoma to BCL2 inhibition. Sci Rep. 2017 Dec 21;7(1):18007. DOI:10.1038/s41598-017-18368-w

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